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编 号：F195430
分子式：C26H21N5O2
分子量：435.48
分子式：C26H21N5O2
分子量：435.48
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CAS No: 1627716-22-6
产品详情
生物活性：
CD161 (NKR-P1A) is a potent, selective and orally bioavailable bromodomain and extra-terminal (BET) bromodomain inhibitor with an IC50s of 28.2 nM and 7.2 nM for BRD4 BD1 and BRD4 BD2, respectively. CD161 has good anticancer activity.
体内研究：
CD161 (NKR-P1A) (po; 20, 40 mg/kg/day; 45 days) achieves essentially complete tumor growth inhibition.CD161 (5 mg/kg (iv), 25 mg/kg (po); 0-24 hours) has the t1/2 of 2.4 hours (iv) and 2.9 hours (po) for rat; the Cmax of 7333 ng/mL (po) for rat. The t1/2 of mice is 0.5 hours (iv) and 1.60 hours (po); the Cmax of mice is 983.1 ng/mL (po) . Animal Model:Dorsal side of severe combined immunodeficient (SCID) mice
Dosage:20, 40 mg/kg
Administration:Po; daily; 45 days
Result:Achieved essentially complete tumor growth inhibition.
Animal Model:Rat or mice
Dosage:5 mg/kg (iv), 25 mg/kg (po) for rat and mice (Pharmacokinetic Study)
Administration:Iv and po; 0, 5, 15, 30 mins, and 1, 2, 4, 6, 8, 24 hours
Result:The t1/2 of rat is 2.4 hours (iv) and 2.9 hours (po); the Cmaxof rat is 7333 ng/mL (po). The t1/2 of mice is 0.5 hours (iv) and 1.60 hours (po); the Cmax of mice is 983.1 ng/mL (po) .
体外研究：
CD161 (NKR-P1A) has Kis of 8.2 nM and 1.4 nM for BRD4 BD1 and BRD4 BD2, respectively. CD161 (30-3000 nM; 1 hours) is very effective in inducing rapid down-regulation of c-Myc at as early as the 1 h time point and in a dose-dependent manner.
CD161 (NKR-P1A) is a potent, selective and orally bioavailable bromodomain and extra-terminal (BET) bromodomain inhibitor with an IC50s of 28.2 nM and 7.2 nM for BRD4 BD1 and BRD4 BD2, respectively. CD161 has good anticancer activity.
体内研究：
CD161 (NKR-P1A) (po; 20, 40 mg/kg/day; 45 days) achieves essentially complete tumor growth inhibition.CD161 (5 mg/kg (iv), 25 mg/kg (po); 0-24 hours) has the t1/2 of 2.4 hours (iv) and 2.9 hours (po) for rat; the Cmax of 7333 ng/mL (po) for rat. The t1/2 of mice is 0.5 hours (iv) and 1.60 hours (po); the Cmax of mice is 983.1 ng/mL (po) . Animal Model:Dorsal side of severe combined immunodeficient (SCID) mice
Dosage:20, 40 mg/kg
Administration:Po; daily; 45 days
Result:Achieved essentially complete tumor growth inhibition.
Animal Model:Rat or mice
Dosage:5 mg/kg (iv), 25 mg/kg (po) for rat and mice (Pharmacokinetic Study)
Administration:Iv and po; 0, 5, 15, 30 mins, and 1, 2, 4, 6, 8, 24 hours
Result:The t1/2 of rat is 2.4 hours (iv) and 2.9 hours (po); the Cmaxof rat is 7333 ng/mL (po). The t1/2 of mice is 0.5 hours (iv) and 1.60 hours (po); the Cmax of mice is 983.1 ng/mL (po) .
体外研究：
CD161 (NKR-P1A) has Kis of 8.2 nM and 1.4 nM for BRD4 BD1 and BRD4 BD2, respectively. CD161 (30-3000 nM; 1 hours) is very effective in inducing rapid down-regulation of c-Myc at as early as the 1 h time point and in a dose-dependent manner.
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